Activating Compound | Comment | Organism | Structure |
---|---|---|---|
17alpha-ethynylestradiol | slightly activates the 3-beta-glucuronidation of estradiol to 116% at 0.005 mM, but inhibits it at 0.1 mM by 23% | Homo sapiens | |
propofol | activates the glucuronidation of 4-methylumbelliferone at 0.2 mM leading to 1.5fold increased Vmax and 0.53fold reduced Km, overview | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
17alpha-ethynylestradiol | slightly activates the 3-beta-glucuronidation of estradiol to 116% at 0.005 mM, but inhibits it at 0.1 mM by 23%, inhibits glucuronidation of 4-methylumbelliferone at all concentration of 0.1 mM | Homo sapiens | |
propofol | inhibits 3-beta-glucuronidation of estradiol by recombinant isozyme UGT1A1 and by liver microsomes | Homo sapiens |
KM Value [mM] | KM Value Maximum [mM] | Substrate | Comment | Organism | Structure |
---|---|---|---|---|---|
0.054 | - |
4-Methylumbelliferone | pH 7.5, 37°C, 0.2 mM propofol, isozyme UGT1A1 | Homo sapiens | |
0.101 | - |
4-Methylumbelliferone | pH 7.5, 37°C, isozyme UGT1A1 | Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
microsome | - |
Homo sapiens | - |
- |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
UDP-D-glucuronate + acceptor | Homo sapiens | - |
UDP + acceptor beta-D-glucuronoside | - |
? | |
UDP-D-glucuronate + estradiol | Homo sapiens | liver microsomes | UDP + estradiol-3-beta-D-glucuronoside | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P22309 | isozyme UGT1A1; isozyme UGT1A1 | - |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
liver | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
UDP-D-glucuronate + 4-methylumbelliferone | recombinant isozyme UGT1A1 | Homo sapiens | UDP + 4-methylumbelliferyl beta-D-glucuronoside | - |
? | |
UDP-D-glucuronate + acceptor | - |
Homo sapiens | UDP + acceptor beta-D-glucuronoside | - |
? | |
UDP-D-glucuronate + estradiol | liver microsomes | Homo sapiens | UDP + estradiol-3-beta-D-glucuronoside | - |
? | |
UDP-D-glucuronate + estradiol | recombinant isozyme UGT1A1 | Homo sapiens | UDP + estradiol-3-beta-D-glucuronoside | - |
? |
Synonyms | Comment | Organism |
---|---|---|
UDP-glucuronosyltransferase | - |
Homo sapiens |
UGT1A1 | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.5 | - |
assay at | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0086 | - |
pH 7.5, 37°C, inhibition of glucuronidation of 4-methylumbelliferone by isozyme UGT1A1 | Homo sapiens | 17alpha-ethynylestradiol | |
0.059 | - |
pH 7.5, 37°C, inhibition of 3-beta-glucuronidation of estradiol by recombinant isozyme UGT1A1 | Homo sapiens | propofol | |
0.228 | - |
pH 7.5, 37°C, inhibition of 3-beta-glucuronidation of estradiol by liver microsomes | Homo sapiens | propofol |